Epilespsy refers to the many types of recurrent seizures produced by paroxysmal excessive neuronal discharges in the brain. The mainstay of treatment has been the long-term and consistent administration of anticonvulsant drugs. Unfortunately, despite the many available chemotherapeutic agents, none are capable of achieving total seizure control and most have disturbing side effects. Medication remains essentially non-specific and is directed against mechanisms of neuronal hyperexcitability that are poorly understood. Clearly, current therapy has not "seized control" of this debilitating disease, rather the reverse still remains true. Recent pharmacological studies support the concept that incorporation of a vicinal diamino-moiety within a substrate is usually accompanied by increased CNS depressant activity. Currently, few methods of generality exist for the preparation of this group. Our plans call for the initial development of new, general, and regiospecific synthetic methods for the construction of a diamino-moiety within the framework of readily accessible starting materials. Once the basic diamine group has been incorporated in the molecule, a select series of derivatives will be prepared. Emphasis will be placed on strategically incorporating those functional groups which have proven effective in the control of epileptic seizures and in evaluating the effect of ring size and conformation on biological activity. The overall criteria for success is the development of new anticonvulsant agents which have high specificity and low toxicity. Samples will be submitted to the National Institutes of Health Epilepsy Branch screening program for evaluation.